TOPICAL FORMULATION FOR A JAK INHIBITOR
This invention relates to pharmaceutical formulations for topical skin application comprising (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders.
1 . A pharmaceutical formulation for topical skin application, comprising:
an oil-in-water emulsion; and
a therapeutically effective amount of a therapeutic agent which is (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof.
2 . A pharmaceutical formulation according to claim 1 , wherein the emulsion comprises water, an oil component, and an emulsifier component.
3 - 4 . (canceled)
5 . A pharmaceutical formulation according to claim 2 , wherein the oil component is present in an amount of about 20% to about 27% by weight of the formulation.
6 . (canceled)
7 . A pharmaceutical formulation according to claim 2 , wherein the oil component comprises one or more substances independently selected from white petrolatum, cetyl alcohol, stearyl alcohol, light mineral oil, medium chain triglycerides, and dimethicone.
8 . A pharmaceutical formulation according to claim 2 , wherein the oil component comprises an occlusive agent component.
9 . (canceled)
10 . A pharmaceutical formulation according to claim 8 , wherein the occlusive agent component is present in an amount of about 5% to about 10% by weight of the formulation.
11 . (canceled)
12 . A pharmaceutical formulation according to claim 8 , wherein the occlusive agent component comprises white petrolatum.
13 . A pharmaceutical formulation according to claim 2 , wherein the oil component comprises a stiffening agent component.
14 - 15 . (canceled)
16 . A pharmaceutical formulation according to claim 13 , wherein the stiffening agent component is present in an amount of about 4% to about 7% by weight of said formulation.
17 - 18 . (canceled)
19 . A pharmaceutical formulation according to claim 13 , wherein the stiffening agent component comprises one or more substances independently selected from C 16-18 fatty alcohols.
20 . (canceled)
21 . A pharmaceutical formulation according to claim 2 , wherein the oil component comprises an emollient component.
22 . (canceled)
23 . A pharmaceutical formulation according to claim 21 , wherein the emollient component is present in an amount of about 7% to about 13% by weight of the formulation.
24 - 25 . (canceled)
26 . A pharmaceutical formulation according to claim 21 , wherein the emollient component comprises one or more substances independently selected from light mineral oil, medium chain triglycerides, and dimethicone.
27 - 28 . (canceled)
29 . A pharmaceutical formulation according to claim 2 , wherein the water is present in an amount of about 45% to about 55% by weight of the formulation.
30 - 32 . (canceled)
33 . A pharmaceutical formulation according to claim 2 , wherein the emulsifier component is present in an amount of about 4% to about 7% by weight of the formulation.
34 . (canceled)
35 . A pharmaceutical formulation according to claim 2 , wherein the emulsifier component comprises one or more substances independently selected from glyceryl fatty esters and sorbitan fatty esters.
36 . (canceled)
37 . A pharmaceutical formulation according to claim 2 , wherein said pharmaceutical formulation further comprises a stabilizing agent component.
38 - 39 . (canceled)
40 . A pharmaceutical formulation according to claim 37 , wherein the stabilizing agent component is present in an amount of about 0.3 to about 0.5% by weight of the formulation.
41 . (canceled)
42 . A pharmaceutical formulation according to claim 37 , wherein the stabilizing agent component comprises xanthan gum.
43 . A pharmaceutical formulation according to claim 1 , wherein said pharmaceutical formulation further comprises a solvent component.
44 - 45 . (canceled)
46 . A pharmaceutical formulation according to claim 43 , wherein the solvent component is present in an amount of about 20% to about 25% by weight of the formulation.
47 . A pharmaceutical formulation according to claim 43 , wherein the solvent component comprises one or more substances independently selected from alkylene glycols and polyalkylene glycols.
48 . (canceled)
49 . A pharmaceutical formulation according to claim 1 , wherein the therapeutic agent is present in an amount of about 0.5% to about 1.5% by weight of the formulation on a free base basis.
50 . A pharmaceutical formulation according to claim 1 , wherein said therapeutic agent is present in an amount of about 0.5% by weight of the formulation on a free base basis.
51 . A pharmaceutical formulation according to claim 1 , wherein said therapeutic agent is present in an amount of about 1% by weight of the formulation on a free base basis.
52 . A pharmaceutical formulation according to claim 1 , wherein said therapeutic agent is present in an amount of about 1.5% by weight of the formulation on a free base basis.
53 . A pharmaceutical formulation according to claim 1 , wherein said therapeutic agent is (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile phosphoric acid salt.
54 - 74 . (canceled)
75 . A method of treating a skin disorder in a patient in need thereof, comprising applying a pharmaceutical formulation according to claim 1 to an area of skin of said patient.
76 . (canceled)
77 . The method of claim 75 , wherein the skin disorder is psoriasis.
78 - 82 . (canceled)